Homogenous antibody drug conjugates via enzymatic methods
First Claim
1. An engineered transglutaminase comprising an amino acid sequence having at least about 80% identity to SEQ ID NO:
- 16, wherein the engineered transglutaminase comprises one or more mutations selected from the group consisting of;
deletion of D1-E4;
deletion of P244-P247;
deletion of N282-L285;
substitution of H279-A287 with a G; and
substitution of A280-H289 with a G.
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Accused Products
Abstract
The present application in one aspect provide Fc-containing polypeptide conjugates comprising an Fc-containing polypeptide conjugated to a conjugate moiety, wherein the Fc-containing polypeptide comprises an N-glycosylated Fc region comprising an acceptor glutamine residue flanked by an N-glycosylation site and wherein the conjugate moiety is conjugated to the Fc-containing polypeptide via the acceptor glutamine residue. Also provided are methods of making such Fc-containing polypeptide conjugates by using a wildtype or engineered transglutaminases. Further provided are engineered transglutaminases specifically designed for carrying out such reactions.
16 Citations
15 Claims
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1. An engineered transglutaminase comprising an amino acid sequence having at least about 80% identity to SEQ ID NO:
- 16, wherein the engineered transglutaminase comprises one or more mutations selected from the group consisting of;
deletion of D1-E4;
deletion of P244-P247;
deletion of N282-L285;
substitution of H279-A287 with a G; and
substitution of A280-H289 with a G.
- 16, wherein the engineered transglutaminase comprises one or more mutations selected from the group consisting of;
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2. An engineered transglutaminase comprising an amino acid sequence having at least about 80% identity to SEQ ID NO:
- 17, wherein the engineered transglutaminase comprises one or more mutations selected from the group consisting of;
deletion of P1-E5;
deletion of P245-P248;
deletion of N283-L286;
substitution of H280-A288 with a G; and
substitution of A281-H290 with a G. - View Dependent Claims (3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15)
- 17, wherein the engineered transglutaminase comprises one or more mutations selected from the group consisting of;
Specification